Advancements in Quinazoline Derivatives as Targeted Anticancer Agents: A Review on its Synthesis, Mechanisms, and Therapeutic Potential

Mohd. Javed Naim ¹*

This review highlights the therapeutic potential of quinazoline derivatives in cancer treatment, focusing on their ability to target critical tyrosine kinases and offering insights into their development as effective anticancer agents.

Abstract

This review focuses on the advancements in the design, synthesis, and evaluation of quinazoline derivatives as potential anticancer agents. Quinazoline, a versatile nitrogen-containing heterocyclic compound, has gained significant attention due to its biological activities and its ability to target key kinases involved in cancer progression, such as EGFR, VEGFR-2, JAK2, MPS1, and PLK1. Since 2000, numerous quinazoline-based derivatives have been synthesized, demonstrating varying degrees of anticancer potency against a range of cancer cell lines, including MCF-7, A549, HT-29, and HepG2. These derivatives, modified with functional groups such as aniline, aryloxy, pyrazole, thiazole, and hydroxamic acid, have shown promise as potential alternatives to conventional chemotherapeutic agents. Notably, compounds such as 51, 52, 53, and 62 have exhibited potent anticancer activity with IC50 values ranging from sub-micromolar to micromolar concentrations. The review highlights the significant therapeutic potential of quinazoline derivatives, particularly in targeting tyrosine kinases involved in cell proliferation, survival, and metastasis. Furthermore, the synthesis and structure-activity relationships (SAR) of these compounds are discussed, offering valuable insights for the development of new quinazoline analogues as targeted cancer therapies. Although promising, further studies are needed to refine their clinical efficacy and explore their full potential in diverse cancer models.

Keywords: Quinazoline derivatives, anticancer agents, tyrosine kinases, EGFR, VEGFR-2

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